- Domeniu: Government; Health care
- Number of terms: 6957
- Number of blossaries: 0
- Company Profile:
The National Cancer Institute (NCI) is part of the National Institutes of Health (NIH), which is one of 11 agencies that compose the Department of Health and Human Services (HHS). The NCI, established under the National Cancer Institute Act of 1937, is the Federal Government's principal agency for ...
A small molecule with potential antineoplastic and antiangiogenic activities. NMPRTase inhibitor APO866 binds to and inhibits nicotinamide phosphoribosyltransferase (NMPRTase), inhibiting the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell prioduction of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis. The coenzyme NAD+ plays an essential role in cellular redox reactions, including the redox reaction linking the citric acid cycle and oxidative phosphorylation.
Industry:Pharmaceutical
A small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration.
Industry:Pharmaceutical
A small synthetic molecule of triazolopyrimidine derivative with potential antitumor activity. With a novel mechanism of action distinct from the action of other vinca alkaloid compounds, TTI-237 specifically binds to tubulin at the vinca site, and promotes the polymerization of tubulin into microtubules. TTI-237 stabilizes tubulin and inhibits microtubule disassembly. This results in cell cycle arrest at the G2/M phase, and leading to cell death.
Industry:Pharmaceutical
A small synthetic peptide containing an RGD-sequence (Arg-Gly-Asp) attached to the positron-emitting isotope fluorine F 18 that may be used to selectively image tumor cells and tumor vasculature by PET imaging. The RGD motif of fluorine F 18 RGD-based integrin peptide-polymer AH111585 selectively binds to the alphaVbeta3 integrin receptor, commonly upregulated on the surfaces of tumor cells and tumor vasculature endothelial cells. This agent may be of use in visualizing and quantifying a decrease in tumor vascularity in response to antiangiogenic agents.
Industry:Pharmaceutical
A small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Dalotuzumab binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed. This agent may preferentially bind to and inhibit Aurora B kinase. Aurora kinases, a family of serine-threonine kinases, are important regulators of cellular proliferation and division.
Industry:Pharmaceutical
A small-molecule bis(thio-hydrazide amide) with oxidative stress induction, pro-apoptotic, and potential antineoplastic activities. Elesclomol induces oxidative stress, creating high levels of reactive oxygen species (ROS), such as hydrogen peroxide, in both cancer cells and normal cells. Because tumor cells have elevated levels of ROS compared to normal cells, the increase in oxidative stress beyond baseline levels elevates ROS beyond sustainable levels, exhausting tumor cell antioxidant capacity, which may result in the induction of the mitochondrial apoptosis pathway. Normal cells are spared because the increase in the level of oxidative stress induced by this agent is below the threshold at which apoptosis is induced.
Industry:Pharmaceutical
A small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to and inhibits the activities of Aurora kinases A, B and C, which may result in inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis and are overexpressed by a wide variety of cancer cell types.
Industry:Pharmaceutical
A small-molecule inhibitor of choline kinase alpha (CHKA), with potential antineoplastic activity. TCD-717 targets and binds to CHKA, an enzyme that plays a key role in the synthesis of phosphatidylcholine, the major phospholipid in eukaryotic cell membranes. Blockade of this enzyme induces cells to activate a different route for phospholipid production which causes a toxic effect and eventually leads to cell destruction. CHKA, overexpressed in human cancer cells while only minimally expressed in normal cells, appears to play a significant role in cellular proliferation, evasion of apoptosis, increased cell motility and metastasis.
Industry:Pharmaceutical
A small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses.
Industry:Pharmaceutical
A small-molecule inhibitor of several kinases with potential antineoplastic activity. Multikinase inhibitor AT9283 binds to and inhibits Aurora kinases A and B, JAK2 (Janus kinase 2) and the kinase BCR-ABL, which may result in the inhibition of cellular division and proliferation and the induction of apoptosis in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis; JAK2 is a kinase that transduces signals from the single chain and IL-3 cytokine receptor families, and from the IFN-gamma receptors; BCR-ABL is a fusion protein with tyrosine kinase activity that is commonly found in CML.
Industry:Pharmaceutical
